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Bioorg Med Chem. 2010 Feb 15;18(4):1665-75. doi: 10.1016/j.bmc.2009.12.067. Epub 2010 Jan 4.

Synthesis and biological evaluation of (phenylpiperazinyl-propyl)arylsulfonamides as selective 5-HT(2A) receptor antagonists.

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1
College of Pharmacy & Division of Life & Pharmaceutical Sciences, Ewha Womans University, Seoul 120-750, Republic of Korea.

Abstract

A novel series of 5-HT(2A) ligands that contain a (phenylpiperazinyl-propyl)arylsulfonamides skeleton was synthesized. Thirty-seven N-(cycloalkylmethyl)-4-methoxy-N-(3-(4-arylpiperazin-1-yl)propyl)-arylsulfonamide and N-(4-(4-arylpiperazin-1-yl)butan-2-yl)-arylsulfonamide compounds were obtained. The binding of these compounds to the 5-HT(2A), 5-HT(2C), and 5-HT(7) receptors was evaluated. Most of the compounds showed IC(50) values of less than 100 nM and exhibited high selectivity for the 5-HT(2A) receptor. Among the synthesized compounds, 16a and 16d showed good affinity at 5-HT(2A) (IC(50)=0.7 nM and 0.5 nM) and good selectivity over 5-HT(2C) (50-100 times) and 5-HT(7) (1500-3000 times).

PMID:
20096593
DOI:
10.1016/j.bmc.2009.12.067
[Indexed for MEDLINE]

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